RESOLVING AND TARGETING THE COMPLEX MOLECULAR MECHANISMS UNDERLYING GPCR SIGNALLING

INPHARMA-Based Determination of Ligand Binding Modes at alpha(1)-Adrenergic Receptors Explains the Molecular Basis of Subtype Selectivity

Tasneem M Vaid, David K Chalmers, Daniel J Scott, Paul R Gooley

2020-08-18

The structural poses of ligands that bind weakly to protein receptors are challenging to define. In this work we have studied liga..

Probing the correlation between ligand efficacy and conformational diversity at the ?(1A)-adrenoreceptor reveals allosteric coupling of its microswitches

Feng-Jie Wu, Lisa M Williams, Alaa Abdul-Ridha, Avanka Gunatilaka, Tasneem M Vaid, Martina Kocan, Alice R Whitehead, Michael DW Griffin, Ross AD Bathgate, Daniel J Scott, Paul R Gooley

2020-05-22

G protein–coupled receptors (GPCRs) use a series of conserved microswitches to transmit signals across the cell membrane via an al..

Diazepam is not a direct allosteric modulator of alpha(1)-adrenoceptors, but modulates receptor signaling by inhibiting phosphodiesterase-4

Lisa M Williams, Xiaoji He, Tasneem M Vaid, Alaa Abdul-Ridha, Alice R Whitehead, Paul R Gooley, Ross AD Bathgate, Spencer J Williams, Daniel J Scott

2019-02-01

α1A- and α1B-adrenoceptors (ARs) are G protein-coupled receptors (GPCRs) that are activated by adrenaline and noradrenaline to mod..